Carvacrol Solvent in Spot-on Parasite Formulations

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Solution Overview

Problem

Existing compositions for controlling parasites on animals using neonicotinoids and pyrethroids face challenges such as poor solubility, stability, and side effects due to the use of solvents like N-methylpyrrolidone and dimethyl sulfoxide, which are toxic and cause skin irritation.

Innovation Solution

A composition comprising ≥8.0 wt.-% carvacrol as a solvent, combined with neonicotinoids like imidacloprid and pyrethroids like permethrin, along with optional crystallization inhibitors and development inhibitors, to enhance solubility and stability while minimizing skin penetration and toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high amounts of neonicotinoids and pyrethroids are used to effectively control ticks and fleas, then the efficacy against parasites is improved, but skin irritations and side effects occur

Engineering Contradiction:
Improveefficacy against parasitesVSAvoidskin irritations
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a new solvent system comprising medium-chain triglycerides and caprylic/capric acid triglyceride as intermediary substances that mediate between the active ingredients and the skin. This solvent system allows effective delivery of high amounts of neonicotinoids and pyrethroids while reducing direct skin irritation compared to traditional solvents

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical and chemical parameters of the formulation by using a specific triglyceride-based solvent system with defined viscosity and solubility characteristics. This parameter change enables the formulation to maintain high active ingredient concentrations while improving skin compatibility and reducing irritation

Inventive Principle:
Principle #35Parameter changes

2Productivity

If neonicotinoids and pyrethroids are combined in high amounts to act effectively against parasitic insects, then the parasite control effectiveness is improved, but undesired side-effects such as skin irritations are caused

Engineering Contradiction:
Improveparasite control effectivenessVSAvoidundesired side-effects
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent creates a composite formulation system combining neonicotinoids, pyrethroids, and a specific triglyceride solvent system. This composite material approach allows the synergistic combination of multiple active ingredients at effective concentrations while the triglyceride matrix moderates their interaction with the skin, reducing harmful side effects

Inventive Principle:
Principle #40Composite materials

3Quantity of substance

If active substances are dissolved in traditional solvents like NMP or DMSO, then solubility is improved, but toxic potential and skin penetration increase

Engineering Contradiction:
Improvesolubility of active substancesVSAvoidtoxic potential
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and removes the harmful traditional solvents (NMP, DMSO) from the formulation and replaces them with a triglyceride-based solvent system. This extraction of harmful substances maintains the necessary solubility of active ingredients while eliminating the toxic potential and excessive skin penetration associated with conventional solvents

Inventive Principle:
Principle #2Taking out (Extraction)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The use of carvacrol as a solvent in the composition improves solubility and stability, reduces side effects, and maintains efficacy against parasites like fleas and ticks without systemic absorption, making it safer and more effective than traditional formulations.

Implementation Method 1

The use of carvacrol as a solvent in the composition improves solubility and stability

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentUS11278022B2Spot-on active substance formulation
Publication Date: 2022.03.22 EVERGREEN ANIMAL HEALTH LLC
  • US11278022B2 patent drawing
  • US11278022B2 patent drawing
  • US11278022B2 patent drawing

AI summary

The invention relates to an improved composition for the control of parasites on animals, comprising comparably high amounts of active substances from the group of agonists of the nicotinergic acetylcholine receptors of insects (neonicotinoids) and from pyrethroids in a new and improved formulation comprising carvacrol as a solvent, and optionally additionally further active and/or auxiliary substances. In particular, the invention relates to the use of such compositions for the control of ectoparasites such as, in particular, fleas, ticks and sand flies in pets such as, in particular, in dogs and ferrets.